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Related Concept Videos

Local Anesthetics: Chemistry and Structure-Activity Relationship01:27

Local Anesthetics: Chemistry and Structure-Activity Relationship

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Local anesthetics (LAs) are drugs that induce a temporary loss of sensation in a limited body area, preventing pain. Cocaine was the first local anesthetic discovered in the late 19th century. Cocaine is a benzoic acid ester obtained from the leaves of coca shrubs and was often used for its psychotropic effects. Cocaine was first isolated in 1860 by Albert Niemann. Sigmund Freud studied the physiological actions of cocaine. Carl Koller later introduced it into clinical practice in 1884 as a...
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Local Anesthetics: Common Agents and Their Applications01:23

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Local anesthetics (LAs) are commonly used for various applications in medical and dental procedures. Some of the common agents used are cocaine, lidocaine, and bupivacaine.
Cocaine is an ester of benzoic acid and methylecgogine. It is used to anesthetize and vasoconstrict locally. Currently, it is used primarily for topical applications. It is beneficial for surgeries on the upper respiratory tract, providing anesthesia and shrinking the mucosa. Cocaine in the form of cocaine hydrochloride is...
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Local Anesthetics: Mechanism of Action01:23

Local Anesthetics: Mechanism of Action

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Local anesthetics (LAs) block sensory and motor impulses by inhibiting the sodium channels on the nerve cell membranes. This induces temporary loss of sensation, relieving pain in a specific body area.
Local anesthetics are amphiphilic molecules consisting of a hydrophobic aromatic part linked to a hydrophilic group by an ester or amide linkage. They are weak bases and are usually available as salts, which increases their solubility and stability. Once administered, LAs exist in the body either...
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Local Anesthetics: Clinical Application as Surface, Infiltration, and Conduction Block Anesthesia01:30

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Depending on the target organ, local anesthetics (LAs) can be administered via various routes. In surface anesthesia, LAs are applied directly to the surface of the skin or mucous membranes. It is widely used for topical skin numbing before venipuncture or minor surgical procedures. Commonly used surface local anesthetics are lidocaine or benzocaine sprays or creams. Surface anesthesia occurs within 5 minutes and lasts for about 60 minutes. One of the main disadvantages of topical anesthesia is...
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Local Anesthetics: Clinical Application as Intravenous Regional Anesthesia01:16

Local Anesthetics: Clinical Application as Intravenous Regional Anesthesia

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Intravenous regional anesthesia or the Bier block technique is used to anesthetize a specific limb or extremity. It uses exsanguinated or blood-drained vessels to transport local anesthetics or LAs to the peripheral nerve trunks. Lidocaine without vasoconstrictors like epinephrine is most commonly used for this technique. Other drugs used are prilocaine, ropivacaine, and chloroprocaine. Bupivacaine is not recommended for this technique due to its high cardiac toxicity.
One of the advantages of...
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Local Anesthetics: Pharmacokinetics01:13

Local Anesthetics: Pharmacokinetics

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The potency and duration of action of local anesthetics (LAs) are determined by their pharmacokinetics. Pharmacokinetics describes how LAs are absorbed, distributed, metabolized, and eliminated from the body. When administered to the vascular tissues, LAs are quickly absorbed and enter the systemic circulation, reducing their localized effects. Adding vasoconstrictors such as epinephrine to LAs reduces their absorption into the systemic circulation, making them clinically effective. The...
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Topical Airway Anesthesia for Awake-endoscopic Intubation Using the Spray-as-you-go Technique with High Oxygen Flow
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Benzonatate as a local anesthetic.

Anna McGuire1,2, Claire A Ostertag-Hill1,2, Gil Aizik1,3

  • 1Laboratory for Biomaterials and Drug Delivery, Boston Children's Hospital, Harvard Medical School, Harvard Institutes of Medicine, Boston, Massachusetts, United States of America.

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Benzonatate demonstrates local anesthetic properties, causing peripheral nerve blockade in rats. However, this cough medicine also induces significant muscle toxicity, limiting its therapeutic potential.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Toxicology

Background:

  • Benzonatate is an FDA-approved antitussive agent.
  • Its chemical structure is similar to known local anesthetics like tetracaine.
  • In vitro studies suggest benzonatate affects voltage-gated sodium channels.

Purpose of the Study:

  • To investigate the potential of benzonatate as a peripheral nerve local anesthetic.
  • To assess its efficacy in producing sensory and motor blockade.
  • To evaluate its myotoxicity and interaction with other agents.

Main Methods:

  • Rats underwent sciatic nerve injection of benzonatate.
  • Sensory and motor blockade were measured using hot plate and weight-bearing tests.
  • Myotoxicity was assessed via histological analysis; effects of co-injection with tetrodotoxin and Tween 80 were examined.

Main Results:

  • Benzonatate induced dose-dependent sensory and motor nerve blockade.
  • Co-administration with tetrodotoxin or Tween 80 prolonged sensory blockade.
  • Histological examination revealed significant inflammation and myotoxicity, even at low concentrations.

Conclusions:

  • Benzonatate functions as a peripheral local anesthetic, causing sensory and motor nerve blockade.
  • It interacts with tetrodotoxin and Tween 80 to extend nerve blockade duration.
  • Significant myotoxicity observed with benzonatate limits its clinical utility as a local anesthetic.